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MALT1 paracaspase inhibitor 3

Chemical Structure : MALT1 paracaspase inhibitor 3

CAS No.: 2088355-90-0

MALT1 paracaspase inhibitor 3 (MALT1 inhibitor)

Catalog No.: PC-35426Not For Human Use, Lab Use Only.

MALT1 paracaspase inhibitor 3 is a potent, specific, covalent inhibitor of MALT1 paracaspase with Ki of 10 nM, exhibits 10-and 100-fold improved potency in vitro and in vivo compared with Z-VRPR-fmk.

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    Biological Activity

    MALT1 paracaspase inhibitor 3 is a potent, specific, covalent inhibitor of MALT1 paracaspase with Ki of 10 nM, exhibits 10-and 100-fold improved potency in vitro and in vivo compared with Z-VRPR-fmk.
    MALT1 paracaspase inhibitor 3 binds covalently to the catalytic cysteine (C464) of MALT1, induces MALT1 oligomerization.
    MALT1 paracaspase inhibitor 3 exhibits potent activity in the Raji-GloSensor MALT1 protease inhibition (IC50=60 nM) and OCI-Ly3 growth inhibition assays (IC50=0.1 uM), selectively inhibits the growth of MALT1 dependent cell lines by decreasing cell proliferation and increasing apoptosis.
    MALT1 paracaspase inhibitor 3 downregulated IL10 protein expression in vitro and in vivo, also decreases STAT3 phosphorylation in ABC DLBCL cells; suppresses the growth of ABC DLBCL tumors in vivo.

    Physicochemical Properties

    M.Wt 569.476
    Formula C24H34BrFN6O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (S)-1-((4-bromobenzoyl)-L-valyl)-N-((S)-1-fluoro-6-guanidino-2-oxohexan-3-yl)pyrrolidine-2-carboxamide

    References

    1. Fontán L, et al. J Clin Invest. 2018 Jul 19. pii: 99436.

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